CNS Sedative-Hypnotics Overview
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Questions and Answers

Which benzodiazepine is classified as a short-acting agent?

  • Midazolam (Versed) (correct)
  • Oxazepam
  • Lorazepam (Ativan)
  • Diazepam

What is the primary action of benzodiazepines on the central nervous system?

  • Inhibit neurotransmitter release
  • Increase neuronal excitability
  • Enhance the effect of GABA (correct)
  • Suppress REM sleep significantly

Which statement correctly identifies an indication for benzodiazepines?

  • Treatment of acute bacterial infections
  • Chronic pain management
  • Management of severe hypertension
  • Induction of sedation in patients with insomnia (correct)

Which adverse effect is commonly associated with benzodiazepines?

<p>Drowsiness (A)</p> Signup and view all the answers

What should clients be instructed to avoid while taking benzodiazepines?

<p>Alcohol (C)</p> Signup and view all the answers

What role does flumazenil serve in benzodiazepine therapy?

<p>It serves as a benzodiazepine receptor antagonist. (D)</p> Signup and view all the answers

Which herb is known to increase CNS depression when combined with benzodiazepines?

<p>Kava (D)</p> Signup and view all the answers

What type of drug is zolpidem (Ambien) categorized as?

<p>Benzodiazepine-like drug (A)</p> Signup and view all the answers

What effect do sedatives have on the CNS?

<p>They reduce nervousness, excitability, and irritability. (C)</p> Signup and view all the answers

What factor distinguishes a sedative from a hypnotic?

<p>The dose at which they are administered. (D)</p> Signup and view all the answers

Which of the following statements accurately describes barbiturates?

<p>They can be used to raise the seizure threshold. (A)</p> Signup and view all the answers

What is a significant risk associated with barbiturate overdose?

<p>Respiratory depression. (D)</p> Signup and view all the answers

Benzodiazepines are commonly preferred over barbiturates due to which of the following reasons?

<p>Better adverse effects profile. (B)</p> Signup and view all the answers

What is a characteristic mechanism of action of barbiturates?

<p>Potentiating GABA action. (D)</p> Signup and view all the answers

What is a consequence of rapid tolerance development in barbiturate use?

<p>Potential for abuse and respiratory depression. (A)</p> Signup and view all the answers

Which classification of benzodiazepines involves medications that alleviate anxiety?

<p>Anxiolytics. (B)</p> Signup and view all the answers

Which benzodiazepine is known for its intermediate acting properties?

<p>Lorazepam (Ativan) (D)</p> Signup and view all the answers

What is a primary advantage of benzodiazepines over barbiturates?

<p>They do not increase the metabolism of other drugs. (D)</p> Signup and view all the answers

Which statement correctly describes the side effect of 'paradoxical excitement' in benzodiazepine use?

<p>It results in increased nervousness and agitation. (C)</p> Signup and view all the answers

Which of the following is NOT a common effect of benzodiazepines?

<p>Aggression (B)</p> Signup and view all the answers

What interaction does grapefruit juice have with benzodiazepines?

<p>It alters their drug absorption. (C)</p> Signup and view all the answers

Which benzodiazepine can be used as a reverse agent in case of an overdose?

<p>Flumazenil (B)</p> Signup and view all the answers

What is a distinguishing feature of sedative-hypnotics at low doses?

<p>They reduce CNS function without causing sleep. (D)</p> Signup and view all the answers

Which of the following statements about barbiturates is correct?

<p>They can raise the seizure threshold, reducing seizures. (C)</p> Signup and view all the answers

What can occur following the discontinuation of benzodiazepines after long-term use?

<p>Rebound insomnia. (B)</p> Signup and view all the answers

What is a common consequence of barbiturate overdose?

<p>Respiratory depression leading to respiratory arrest. (C)</p> Signup and view all the answers

Which of the following substances should be avoided by clients taking benzodiazepines?

<p>Alcohol (C)</p> Signup and view all the answers

Why are benzodiazepines preferred over barbiturates as sedative-hypnotics?

<p>They have a better pharmacological and adverse effects profile. (B)</p> Signup and view all the answers

What characterizes the mechanism of action of barbiturates?

<p>They mimic GABA and potentiate its action. (B)</p> Signup and view all the answers

Which type of agent is commonly associated with long-term benzodiazepine use?

<p>Both anxiolytic and sedative-hypnotic. (A)</p> Signup and view all the answers

What is a potential risk associated with the clinical use of barbiturates?

<p>They can induce liver enzyme production. (B)</p> Signup and view all the answers

What effect can benzodiazepines have at higher doses?

<p>Induction of sleep similar to barbiturates. (D)</p> Signup and view all the answers

Flashcards

Sedative

A drug that reduces nervousness, excitability, and irritability without causing sleep.

Hypnotic

A drug that reduces CNS function to induce sleep.

Sedative-Hypnotic

A drug that can act as either a sedative or hypnotic depending on the dose.

Barbiturates

A class of drugs that act as sedative-hypnotics, antiepileptics, and anesthetics.

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Therapeutic Index

A measure of a drug's safety, reflecting the ratio between the effective dose and the toxic dose.

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Benzodiazepines

The most commonly prescribed sedative-hypnotic and anxiolytic drug class.

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Benzodiazepines: Sedative-Hypnotic

Benzodiazepines used to induce sleep.

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Benzodiazepines: Anxiolytic

Benzodiazepines used to relieve anxiety.

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GABA's role in CNS

Gamma-aminobutyric acid (GABA) is a neurotransmitter that inhibits neuronal activity in the central nervous system (CNS), reducing excitability and promoting relaxation.

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Benzodiazepines: Mechanism

Benzodiazepines enhance the effects of GABA by binding to specific receptors on neurons, leading to increased inhibition and reduced neuronal excitability.

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Benzodiazepines: CNS effects

Benzodiazepines depress CNS activity, leading to effects like sedation, sleep induction, muscle relaxation, and anxiety relief.

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Benzodiazepines: Sleep impact

Benzodiazepines do not suppress REM sleep as much as barbiturates, making them less likely to cause rebound insomnia.

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Benzodiazepines: PO vs IV

Oral administration of benzodiazepines does not significantly depress respiration, but IV administration can depress respiration especially when combined with other CNS depressants.

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Flumazenil: Benzodiazepine antidote

Flumazenil is a benzodiazepine receptor antagonist used to reverse benzodiazepine overdose.

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Benzodiazepines: Indications

Benzodiazepines are used for various conditions, including sedation, sleep induction, muscle relaxation, anxiety relief, alcohol withdrawal, agitation, epilepsy, and balanced anesthesia.

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Benzodiazepines: Adverse Effects

Common adverse effects of benzodiazepines include drowsiness, headache, dizziness, vertigo, lethargy, and paradoxical excitement.

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Barbiturate Mechanism

Barbiturates act by potentiating the effects of GABA, a neurotransmitter that inhibits nerve activity. They both mimic and enhance the action of GABA, leading to a calming effect.

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Barbiturate Toxicity

Overdose of barbiturates can be dangerous, leading to respiratory depression and even death. This is due to their powerful ability to suppress breathing.

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Benzodiazepine Toxicity

Compared to barbiturates, benzodiazepines are generally safer in terms of overdose. Flumazenil can be used as an antidote to reverse benzodiazepine overdose.

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Barbiturate Therapeutic Index

Barbiturates have a narrow therapeutic index, meaning the difference between a therapeutic dose and a toxic dose is small. Careful monitoring is critical for barbiturate use.

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Benzodiazepine Therapeutic Index

Benzodiazepines generally have a wider therapeutic index compared to barbiturates, making them considered safer in regards to dosage.

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Benzodiazepine action

Benzodiazepines enhance the effect of GABA, a neurotransmitter that inhibits nerve activity, leading to a decrease in neuronal excitability and CNS depression.

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Benzodiazepine effect on sleep

Benzodiazepines do not suppress REM sleep as much as barbiturates, minimizing the risk of rebound insomnia.

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Benzodiazepine route: PO vs IV

Oral (PO) benzodiazepines generally do not significantly depress respiration, but intravenous (IV) administration can depress respiration, especially when combined with other CNS depressants.

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Flumazenil

Flumazenil is a benzodiazepine receptor antagonist used to reverse benzodiazepine overdose.

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Benzodiazepine interactions?

Benzodiazepines interact with other CNS depressants (alcohol, opioids), grapefruit juice, cimetidine (a drug for ulcers), and certain herbs.

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Benzodiazepine client care

Instruct clients to avoid alcohol and other CNS depressants. Gradual dose reduction is essential to prevent rebound insomnia after prolonged use.

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Benzodiazepine withdrawal

Discontinuing benzodiazepine use abruptly can lead to rebound insomnia, anxiety, tremors, and seizures.

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Zolpidem (Ambien)

Zolpidem is a non-benzodiazepine hypnotic that works on the same brain receptors as benzodiazepines, used for short-term management of insomnia.

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Study Notes

CNS Sedative-Hypnotics

  • CNS sedative-hypnotics are drugs that depress the central nervous system (CNS).
  • Sedatives reduce nervousness, excitability, and irritability without causing sleep.
  • Hypnotics reduce CNS function to the point of inducing sleep.
  • A sedative can become a hypnotic in high enough doses.
  • Sedative-hypnotics are often used in lower doses to reduce symptoms, and higher doses to induce sleep.

CNS Depressants: Barbiturates

  • Barbiturates are sedative-hypnotics.
  • They're now rarely used as hypnotics but lower doses are sometimes still used.
  • They are useful as antiepileptics, raising seizure thresholds to reduce seizures.
  • They are also used in anesthesia for short procedures.
  • Specific examples of short-acting barbiturates include pentobarbital (rarely used).
  • Examples of long-acting barbiturates include phenobarbital (often used as an antiepileptic).
  • Barbiturates have a narrow therapeutic index; blood levels must be carefully monitored.
  • Mechanism of action: They broadly depress the CNS and potentiate/mimic the actions of GABA.
  • Metabolism occurs in the liver and they're excreted in urine.
  • Toxicity includes respiratory depression. Overdose can lead to respiratory arrest, coma, and death.
  • Barbiturates are less commonly used due to tolerance, physical dependence, liver enzyme induction, abuse potential, powerful respiratory depression, and lack of an antidote.

CNS Depressants: Benzodiazepines

  • Benzodiazepines are the most commonly prescribed sedative-hypnotics (and anxiolytics).
  • They have favorable adverse effect profiles compared to barbiturates.
  • They offer good efficacy and safety.
  • They are classified as sedative-hypnotics and anxiolytics.
  • Long-acting examples include chlordiazepoxide, clorazepate, and flurazepam.
  • Intermediate-acting examples include lorazepam (Ativan) and oxazepam.
  • Short-acting examples include midazolam (Versed, IV) and triazolam.
  • Mechanism of action: Benzodiazepines enhance the effect of GABA, decreasing neuronal excitability and depressing CNS activity.
  • They affect hypothalamic, thalamic, and limbic brain systems.
  • Unlike barbiturates, they do not suppress REM sleep or increase metabolism of other drugs.
  • They do not severely depress respiration in oral doses, though this can occur in overdose, particularly when combined with other CNS depressants or given intravenously.
  • Flumazenil is a benzodiazepine receptor antagonist used to reverse benzodiazepine overdose.

Benzodiazepines: Indications

  • Sedation
  • Sleep induction
  • Skeletal muscle relaxation
  • Anxiety relief
  • Alcohol withdrawal treatment
  • Agitation
  • Epilepsy
  • Balanced anesthesia

Benzodiazepines: Adverse Effects

  • Drowsiness
  • Headache
  • Dizziness
  • Vertigo
  • Lethargy
  • Paradoxical excitement
  • "Hangover" effect

Benzodiazepines: Interactions

  • All other CNS depressants (e.g. alcohol, opioids) have cumulative effects.
  • Grapefruit juice alters drug absorption.
  • Cimetidine inhibits benzodiazepine metabolism.
  • Herbs like kava, valerian, and chamomile increase CNS depression.

Client Care Implications

  • Clients should avoid alcohol and other CNS depressants.
  • Rebound insomnia may occur after stopping the medication, so dosages should be reduced gradually.

Other Hypnotics

  • BZD-like drugs (e.g., zolpidem (Ambien), zaleplon, zopiclone) are structurally different from benzodiazepines but act on the same drug target..
  • These are used for short-term insomnia treatment.

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CNS Depressants Class PDF

Description

Explore the world of CNS sedative-hypnotics, including their functions, uses, and classifications. Learn about the sedative and hypnotic properties of these medications, specifically focusing on barbiturates and their applications in reducing seizures and anesthesia. This quiz will enhance your understanding of this critical area in pharmacology.

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